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Use of a Design of Experiments approach for the optimisation of a microwave assisted Ugi reaction

Heather Tye* and Mark Whittaker

*Evotec OAI, Milton Park, Abingdon, Oxfordshire, UK OX14 4SD, Email: heather.tyeevotecoai.com

H. Tye, M. Whittaker, Org. Biomol. Chem., 2004, 2, 813-815.

DOI: 10.1039/b400298a


Abstract

The utility of a Design of Experiments (DoE) approach for the rapid and efficient optimisation of a microwave assisted Ugi 3cc reaction of levulinic acid with a range of amine and isonitrile substrates has enabled the preparation of lactam derivatives in moderate to excellent yields in a reaction time of only 30 min compared to the conventional methodology which required up to 48 h.

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Key Words

Ugi Reaction, Microwave Synthesis, Multicomponent Reactions, γ-Lactams


ID: J52-Y2004-210